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Inside Back Cover: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. Int. Ed. 30/2015)
Author(s) -
Frett Brendan,
Carlomagno Francesca,
Moccia Maria Luisa,
Brescia Annalisa,
Federico Giorgia,
De Falco Valentina,
Admire Brittany,
Chen Zhongzhu,
Qi Wenqing,
Santoro Massimo,
Li Hongyu
Publication year - 2015
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201505540
Subject(s) - vegf receptors , int , kinase , cover (algebra) , dual (grammatical number) , chemistry , cancer research , pharmacology , medicine , biochemistry , computer science , philosophy , mechanical engineering , engineering , operating system , linguistics
The inhibitory powers of a next‐generation inhibitor were carefully balanced so that it is equally potent on the RET kinase and VEGFR 2 . In their Communication on page 8717 ff., H.‐y. Li, M. Santoro, et al. report the optimization of a dual inhibitor for the treatment of RET‐driven malignancies through synergistic medicinal chemistry. The inhibitor is capable of simultaneously treating the parenchyma (RET) and stroma (VEGFR 2 ) at the same therapeutic dose.